PMID: 43552Jan 1, 1979

Single- and multiple-dose kinetics of estazolam, a triazolo benzodiazepine

Psychopharmacology
M D AllenJ D Arnold

Abstract

The pharmacokinetic properties of estazolam, a triazolo benzodiazepine hypnotic agent, were assessed in a series of healthy volunteers following single and multiple doses. After single oral doses of 2--16 mg, peak plasma concentrations were reached within 6 h. Values of elimination half-life ranged from 8.3--31.2 h (mean 17.0 h) and did not vary significantly with dose. During 3 weeks of therapy, steady-state plasma concentrations increased approximately in proportion to increasing doses. and accumulation was essentially complete within 3 days of each dose change. The mean observed accumulation ratio was 1.84, which was slightly larger than the predicted ratio of 1.53. Exposure to multiple-dose estazolam therapy had no significant influence on the kinetics of a single dose of antipyrine, suggesting that estazolam neither stimulates nor inhibits enzyme activity in humans. Thus the accumulation and elimination kinetics of estazolam can be classified as intermediate to those of the short-acting (such as oxazepam) and the long-acting (such as diazepam) benzodiazepine derivatives.

References

Aug 1, 1978·Southern Medical Journal·D J Greenblatt, R I Shader
Jan 1, 1979·Journal of Pharmaceutical Sciences·D J GreenblattE Woo
Jan 1, 1979·Annual Review of Pharmacology and Toxicology·D J Greenblatt
Aug 1, 1975·The Journal of Infectious Diseases·M BarzaL Weinstein
Jun 1, 1975·Journal of Pharmacokinetics and Biopharmaceutics·K S AlbertJ G Wagner
Oct 2, 1975·The New England Journal of Medicine·D J Greenblatt, J Kock-Weser
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Nov 7, 1974·The New England Journal of Medicine·D J Greenblatt, R I Shader
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Citations

Jun 1, 1990·Journal of Clinical Pharmacology·J B SkatrudD Juan
Aug 1, 1991·Journal of Clinical Pharmacology·J B CohnM Ettinger
Mar 1, 1987·Pharmacology, Biochemistry, and Behavior·C E Johanson
Nov 17, 1993·Journal of Chromatography·J F Kelly, D J Greenblatt
May 31, 2002·Analytical Sciences : the International Journal of the Japan Society for Analytical Chemistry·Masatomo MiuraKoichi Otani
Jan 1, 1983·Drug Metabolism Reviews·D J GreenblattR I Shader
Jan 1, 1984·Current Medical Research and Opinion·R Jochemsen, D D Breimer
Mar 2, 1990·The American Journal of Medicine·D J GreenblattR I Shader
Mar 2, 1990·The American Journal of Medicine·L E Gustavson, P J Carrigan
Mar 1, 1985·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·A MancinelliS Caccia
Apr 1, 1997·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·L Dal BoM L De Vito
Mar 1, 1983·Klinische Wochenschrift·H R Ochs
Mar 1, 1997·Journal of Anesthesia·Yuichi Kanmura, Mutumi Kamihashi
Jan 1, 1986·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·J M MachinistD Rollins
Jan 1, 1981·British Journal of Clinical Pharmacology·D J GreenblattJ S Harmatz

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